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Search Results for " cb1 agonist 1 "

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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T62761	CB1 agonist 1	Cannabinoid Receptor	GPCR/G Protein
	CB1 agonist 1 是一种有效的 CB1 激动剂，对 CB1 受体的 pIC50 值为 5.7。CB1 agonist 1可以用于研究大脑失调、疼痛和炎症。
T10694	CB1 inverse agonist 1 MRL-650	Cannabinoid Receptor	GPCR/G Protein
	CB1 inverse agonist 1 (MRL-650) 是一种具有口服活性和选择性的 CB1 激动剂。 CB1 和 CB2 的 IC50 分别为 7.5 nM 和 4100 nM。 CB1 inverse agonist 1 显示出厌食作用。
T62468	CB1/2 agonist 1
	CB1/2 agonist 1 是一种有效的、能够透过血脑屏障的 CB1/2 激动剂，能够作用于 CB1R (EC50: 56.15 nM) 和 CB2R (EC50: 11.63 nM)。CB1/2 agonist 1 能够降低谷氨酸释放，并减少 LPS 诱导的小胶质细胞活化，具有抗炎和镇痛活性。CB1/2 agonist 1 具有潜力进行多发性硬化症的研究。
T62411	CB1/2 agonist 4
	CB1/2 agonist 4 (compound 24) 是一种 CB1 完全激动剂 (EC50: 15.09 nM) ，也是一种 CB2 部分激动剂 (EC50: 1.16 nM)。CB1/2 agonist 4 具有显著的抗伤害感受活性，也能够激活大麻素和TRPV1受体 (IC50: 0.8 μM, EC50: 0.12 μM)。
T61736	CB1/2 agonist 3
	CB1/2 agonist 3 (compound 52), a potent non-selective cannabinoid ligand, is a competitive agonist for the CB1/CB2 receptors. It exhibits CB1/CB2 agonistic activity by binding to the human CB1 and CB2 receptors, with Ki values of 5.9 nM and 3.5 nM, respectively [1].
T62180	CB1/2 agonist 2
	CB1/2 agonist 2 (compound 23) 是一种有效的非选择性大麻素 (cannabinoid) 配体，其Ki 分别为 3.5 nM 和 1.2 nM。CB1/2 agonist 2 是一种 CB1 的完全激动剂，也是 CB2 竞争性反向激动剂。CB1/2 agonist 2 表现出抗伤害效果。
T72395	CB1 inverse agonist 2
	CB1inverse agonist 2 是一种口服有效的大麻素受体 CB1反向激动剂。CB1inverse agonist 2 在小鼠模型中，能有效抑制 CP55940 导致的体温失温和厌食情况。
T13080L	Taranabant MK-0364	Cannabinoid Receptor	GPCR/G Protein
	Taranabant (MK-0364) 是一种具有选择性和高效性的 cannabinoid 1 (CB1) 受体反向激动剂，可用于研究肥胖和尼古丁依赖。
T12306	OMDM-5	Cannabinoid Receptor; Endogenous Metabolite; TRP/TRPV Channel	GPCR/G Protein; Membrane transporter/Ion channel; Metabolism
	OMDM-5 是有效的、选择性的anandamide 细胞摄取抑制剂，Ki 为 4.8 μM。它是VR1 (TRPV1)激动剂，EC50为 75 nM，显示出对大麻素 1 型受体 (CB1) 的弱配体活性 (Ki=4.9 μM)。
T1915	AM251	Cannabinoid Receptor; GPR	Endocrinology/Hormones; GPCR/G Protein
	AM251 是一种选择性大麻素1 受体拮抗剂，IC50=8 nM，是一种 GPR55 的激动剂，EC50=39 nM。
T1519L	Rimonabant SR141716,利莫那班	Cannabinoid Receptor; Antibacterial; Acyltransferase	GPCR/G Protein; Metabolism; Microbiology/Virology
	Rimonabant (SR141716) 是一种选择性的、能透过血脑屏障的中心大麻素受体 1 拮抗剂， Ki 值为 1.8 nM。它也能够抑制分枝杆菌膜蛋白 3。
T13081	Taranabant racemate MK-0364 racemate	Cannabinoid Receptor	GPCR/G Protein
	Taranabant racemate is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor.
T27803	LBP-1 LBP1
	LBP-1 is a cannabinoid receptor type 1 (CB1) agonist.
T28657	SAD-448
	SAD-448 is a cannabinoid receptor type 1 (CB1) agonist. SAD-448 controls spasticity via action on the peripheral nerve CB1 receptor.
T61849	AM8936
	AM8936 is a well-balanced and highly potent agonist for the cannabinoid receptor type-1 (CB1) in functional assays, with EC50 values of 8.6 nM and 1.4 nM for the rat CB1 (rCB1) and human CB1 (hCB1) receptors, respectively. It demonstrates a strong affinity for the rat CB1 receptor, exhibiting a K i value of 0.55 nM. In vivo studies have confirmed that AM8936 is a powerful and effective agonist for the CB1 receptor. Due to its therapeutic potential, AM8936 is particularly valuable for research fo...
T14504	BAY 38-7271	Cannabinoid Receptor	GPCR/G Protein
	BAY 38-7271 has strong neuroprotective properties.[1] BAY 38-7271 is selective and highly potent and cannabinoid CB1/CB2 receptor agonist. With Kis of 1.85 nM and 5.96 nM for recombinant human CB1 receptor and CB2 receptor, respectively.
T69740	AMG-315
	AMG-315 is a Potent Endocannabinoid Ligand with Stability to Metabolizing Enzymes. AMG-315 is a chiral arachidonoyl ethanolamide (AEA) analogue or (13S,1′R)-dimethylanandamide. AMG-315 is a high affinity ligand for the CB1 receptor (Ki of 7.8 ± 1.4 nM) that behaves as a potent CB1 agonist in vitro (EC50 = 0.6 ± 0.2 nM). AMG-315 is the first potent AEA analogue with significant stability for all endocannabinoid hydrolyzing enzymes as well as the oxidative enzymes COX-2. AMG-315 will serve as a ...
T38138	ACEA 2'-chloro-AEA,Arachidonoyl 2'-Chloroethylamide
	Arachidonoyl 2-chloroethylamide (ACEA) is a potent and selective cannabinoid (CB) receptor 1 agonist with Ki values of 1.4 and >2,000 nM for CB1 and CB2 receptors, respectively. In whole animal experiments, ACEA induces hypothermia in mice with the same efficacy as arachidonoyl ethanolamide , in spite of its higher affinity for the CB1 receptor. These data have been interpreted to indicate that ACEA may be a substrate for fatty acid amide hydrolase (FAAH), and thus only transiently available in ...
T75799	Hemopressin(human, mouse) TFA	Cannabinoid Receptor	GPCR/G Protein
	Hemopressin TFA，一种衍生自血红蛋白α1链的九肽，最初自大鼠脑匀浆分离。作为口服活性且选择性的CB1大麻素受体反向激动剂，Hemopressin TFA在炎性疼痛模型中具有抗伤害感受效应。
T78083	CB-25	Cannabinoid Receptor	GPCR/G Protein
	CB-25是一种CB1大麻素受体的部分激动剂配体。它能增强Forskolin诱导的癌细胞中cAMP的形成，但在Forskolin诱导的hCB1-CHO细胞中则不显示增强作用。
T38204	GAT229
	GAT229 is a positive allosteric modulator of cannabinoid receptor 1 (CB1) and the S-(-) enantiomer of the CB1 modulator GAT211. It does not activate the receptor on its own but enhances the binding and activity of CB agonists. GAT229 (1 μM) enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing human recombinant CB1 (hCB1), as well as the activity of 2-arachidonoyl glycerol , arachidonoyl ethanolamide , and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 an...
T75798	Hemopressin(rat) TFA
	Hemopressin(rat) TFA，一种衍生自α1-珠蛋白九肽，最初分离自大鼠脑匀浆。该化合物通过口服能有效选择性地作为CB1大麻素受体的反向激动剂，并在炎性疼痛模型中表现出抗伤害感受活性。
T10294	AM9405	5-HT Receptor	GPCR/G Protein; Neuroscience
	AM9405是一种新型的外周活性大麻素1型 (CB1)和5-羟色胺3型受体激动剂。 AM9405抑制回肠和结肠的抽搐收缩，IC50分别为45.71 和 0.076 nM。AM9405 在生理条件下显着减缓小鼠肠道蠕动.
T27809	LEI-101
	LEI-101 是有效的、选择性的、具有口服活性的大麻素CB2受体激动剂。LEI-101对 hCB2 的 pEC50值为 8，对 hERG 的 pKi 值小于 4。LEI-101 与 CB2 受体的结合能力比 CB1 强100 倍。LEI-101 具有炎症及氧化应激相关疾病的治疗潜力。

化合物

CB1 agonist 1

Cat.No: T62761

Target: Cannabinoid Receptor

CB1 inverse agonist 1

Cat.No: T10694

Synonym: MRL-650

Target: Cannabinoid Receptor

CB1/2 agonist 1

Cat.No: T62468

CB1/2 agonist 4

Cat.No: T62411

CB1/2 agonist 3

Cat.No: T61736

CB1/2 agonist 2

Cat.No: T62180

CB1 inverse agonist 2

Cat.No: T72395

Cat.No: T13080L

Synonym: MK-0364

Target: Cannabinoid Receptor

Cat.No: T12306

Target: Cannabinoid Receptor, Endogenous Metabolite, TRP/TRPV Channel

Cat.No: T1915

Target: Cannabinoid Receptor, GPR

Cat.No: T1519L

Synonym: SR141716,利莫那班

Target: Cannabinoid Receptor, Antibacterial, Acyltransferase

Taranabant racemate

Cat.No: T13081

Synonym: MK-0364 racemate

Target: Cannabinoid Receptor

Cat.No: T27803

Synonym: LBP1

Cat.No: T28657

Cat.No: T61849

Cat.No: T14504

Target: Cannabinoid Receptor

Cat.No: T69740

Cat.No: T38138

Synonym: 2'-chloro-AEA,Arachidonoyl 2'-Chloroethylamide

Hemopressin(human, mouse) TFA

Cat.No: T75799

Target: Cannabinoid Receptor

Cat.No: T78083

Target: Cannabinoid Receptor

Cat.No: T38204

Hemopressin(rat) TFA

Cat.No: T75798

Cat.No: T10294

Target: 5-HT Receptor

Cat.No: T27809

Cat. No.	Product Name	Target	Signaling Pathways
T11834	Leelamine hydrochloride	Others	Others
	Leelamine hydrochloride, a tricyclic diterpene extracted from pine tree bark, inhibits the transcriptional activity of the androgen receptor, known to regulate fatty acid synthesis [2,3]. This compound acts as a cannabinoid receptor type 1 (CB1) agonist and suppresses SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells, irrespective of androgen receptor status.

天然产物

Leelamine hydrochloride

Cat.No: T11834

Target: Others

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